Thomas Daniel, Majeti Ravindra
Division of Hematology, Department of Medicine, Cancer Institute, and Institute for Stem Cell Biology and Regenerative Medicine, Stanford University School of Medicine, Stanford, California.
Cancer Discov. 2017 May;7(5):459-461. doi: 10.1158/2159-8290.CD-17-0270.
AG-221 or enasidenib is a first-in-class selective inhibitor of mutated isocitrate dehydrogenase 2 (IDH2) with early demonstrated clinical efficacy in acute myeloid leukemia as a single agent, yet with persistence of mutant clones. Two articles in this issue of provide further insight into the biological activity of AG-221 in promoting differentiation of -mutant cells and reversing aberrant DNA methylation over time, and demonstrating preclinical activity in combination with a targeted FLT3 kinase inhibitor to eliminate -mutant clones. .
AG-221（即恩西地平）是一种首创的选择性突变异柠檬酸脱氢酶2（IDH2）抑制剂，作为单一药物在急性髓系白血病中已早期显示出临床疗效，但仍存在突变克隆。本期的两篇文章进一步深入探讨了AG-221在促进IDH2突变细胞分化、随时间逆转异常DNA甲基化以及与靶向FLT3激酶抑制剂联合消除IDH2突变克隆方面的生物学活性。
